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21. 发明授权

US4321385A [(Aryl-1-pyrryl) methyl]-piperidinols and pyrrolidinols 失效
标题翻译： [（芳基-1-吡咯基）甲基] - 哌啶醇和吡咯烷醇
公开(公告)号：US4321385A
公开(公告)日：1982-03-23
申请号：US207536
申请日：1980-11-17
申请人： Richard C. Effland , Larry Davis , Joseph T. Klein
发明人： Richard C. Effland , Larry Davis , Joseph T. Klein
IPC分类号： C07D207/32 , C07D207/325 , C07D491/10 , C07D491/107 , C07D401/06 , C07D403/06
CPC分类号： C07D207/325 , C07D491/10
摘要： Compounds of the formula ##STR1## wherein Y is halogen; R is hydrogen, alkyl, alkoxycarbonyl, phenoxycarbonyl, cyano, aralkyl, alkanoyl, aralkanoyl, hydroxyalkyl, benzoylalkyl, ##STR2## where p is an integer of 2 or 3; and R.sub.1 and R.sub.2 are the same or different and are hydrogen and lower alkyl; X is hydrogen and alkyl; Hal is a halogen; q is an integer of 0 or 1; m is an integer of 1 or 2 and n is an integer of 1, 2 or 3, where the sum of m and n is 3 or 4; and a pharmaceutically acceptable acid addition salt thereof, are provided. The compounds are useful intermediates in the preparation of Spiro[dihydrobenzofuran-piperidines and pyrrolidines], which are useful agents for relieving pain and for lowering blood pressure.
摘要翻译：其中Y是卤素的式IMAMA的化合物; R是氢，烷基，烷氧基羰基，苯氧基羰基，氰基，芳烷基，烷酰基，芳烷酰基，羟基烷基，苯甲酰基烷基，其中p是2或3的整数; 且R 1和R 2相同或不同，为氢和低级烷基; X是氢和烷基; 卤素是卤素; q是0或1的整数; m为1或2的整数，n为1,2或3的整数，m和n之和为3或4; 及其药学上可接受的酸加成盐。这些化合物是制备螺[二氢苯并呋喃 - 哌啶和吡咯烷]的有用中间体，它们是缓解疼痛和降低血压的有用药物。

22. 发明授权

US5405856A Certain nitro-3-pyrinamines and 3-oxy-analogues 失效
标题翻译：某些硝基-3-吡啶胺和3-氧基 - 类似物
公开(公告)号：US5405856A
公开(公告)日：1995-04-11
申请号：US42502
申请日：1993-04-02
申请人： Richard C. Effland , Joseph T. Klein , Gordon E. Olsen , Larry Davis , Russell R. L. Hamer , Brian S. Freed
发明人： Richard C. Effland , Joseph T. Klein , Gordon E. Olsen , Larry Davis , Russell R. L. Hamer , Brian S. Freed
IPC分类号： C07D213/74 , C07D213/89 , C07D401/12 , C07D403/12 , A61K31/44 , C07D213/61 , C07D213/72 , C07D213/75
CPC分类号： C07D213/74 , C07D213/89 , C07D401/12 , C07D403/12
摘要： There are described compounds of the formula ##STR1## where n is 0 or 1;X is O or NR.sub.2, R.sub.2 being hydrogen, loweralkyl or loweralkylcarbonyl;R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl; andR.sub.1 is ##STR2## wherein R.sub.3 is hydrogen, loweralkyl or loweralkylcarbonyl;m is 1 or 2;eachR.sub.4 is independently hydrogen or loweralkyl; andY is hydrogen, halogen, loweralkyl, loweralkoxy or trifluoromethyl;which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.
摘要翻译：描述式为“IMAGE”的化合物，其中n为0或1; X是O或NR 2，R 2是氢，低级烷基或低级烷基羰基; R是氢，低级烷基，芳基低级烷基或低级烷基羰基; 并且R1是其中R3是氢，低级烷基或低级烷基羰基; m为1或2; 每个R 4独立地是氢或低级烷基; Y为氢，卤素，低级烷基，低级烷氧基或三氟甲基; 哪些化合物可用作治疗各种皮肤病的局部抗炎剂。

23. 发明授权

US5166163A 3-(1H-indazol-3-yl)-4-pyridinamines 失效
标题翻译： 3-（1H-吲唑-3-基）-4-吡啶胺
公开(公告)号：US5166163A
公开(公告)日：1992-11-24
申请号：US694973
申请日：1991-05-06
申请人： Richard C. Effland , Joseph T. Klein
发明人： Richard C. Effland , Joseph T. Klein
IPC分类号： C07D213/73 , C07D213/75 , C07D401/04
CPC分类号： C07D213/73 , C07D213/75 , C07D401/04
摘要： This invention relates to 3-(1H-indazol-3-yl)-4-pyridinamines of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, arylalkyl or acyl; R.sub.2 is hydrogen, loweralkyl or arylalkyl; R.sub.3 is hydrogen, loweralkyl or aryl and X is hydrogen, halogen, nitro or amino or the pharmaceutically acceptable addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention are useful as analgesics and as topical antiinflammatory agents for the treatment of various dermatoses.
摘要翻译：本发明涉及式（Ia）的3-（1H-吲唑-3-基）-4-吡啶胺，其中R 1是氢，低级烷基，芳烷基或酰基; R2是氢，低级烷基或芳基烷基; R 3是氢，低级烷基或芳基，X是氢，卤素，硝基或氨基或其药学上可接受的加成盐，并且在适用的情况下，其几何和旋光异构体及其外消旋混合物。本发明的化合物可用作止痛剂和用作治疗各种皮肤病的局部抗炎剂。

24. 发明授权

US5102891A 1-(substituted pyridinylamino)-1H-indol-5-yl substituted carbamates 失效
标题翻译： 1-（取代的吡啶基氨基）-1H-吲哚-5-基取代的氨基甲酸酯
公开(公告)号：US5102891A
公开(公告)日：1992-04-07
申请号：US555890
申请日：1990-07-23
申请人： Richard C. Effland , Larry Davis , Gordon E. Olsen , Joseph T. Klein , David G. Wettlaufer , Peter A. Nemoto
发明人： Richard C. Effland , Larry Davis , Gordon E. Olsen , Joseph T. Klein , David G. Wettlaufer , Peter A. Nemoto
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/535 , A61K31/55 , A61P25/28 , A61P43/00 , C07D401/12 , C07D401/14 , C07D413/14 , C12N9/99
CPC分类号： C07D401/12 , C07D401/14
摘要： There are disclosed various compounds of the formula below, ##STR1## where n is 0 or 1;X is hydrogen, halogen, nitro, amino, trifluoromethyl, loweralkyl, or loweralkoxy;Y is hydrogen, halogen, nitro, amino, trifluoromethyl, loweralkyl, or loweralkoxy;R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, loweralkenyl, loweralkynyl, loweralkanoyl, arylloweralkanoyl, heteroarylloweralkyl or heteroarylloweralkanoyl;R.sub.2 is hydrogen, loweralkyl, formyl or cyano;R.sub.3 is hydrogen or loweralkyl;R.sub.4 is loweralkyl, arylloweralkyl, cycloalkyl, aryl or heteroaryl; or alternatively, --NR.sub.3 R.sub.4 taken together constitutes ##STR2## R.sub.5 being hydrogen, loweralkyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl,which compounds are useful for the treatment of various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.
摘要翻译：公开了下式的各种化合物，其中n为0或1; X是氢，卤素，硝基，氨基，三氟甲基，低级烷基或低级烷氧基; Y是氢，卤素，硝基，氨基，三氟甲基，低级烷基或低级烷氧基; R 1是氢，低级烷基，芳基低级烷基，低级烯基，低级炔基，低级烷酰基，芳基低级烷酰基，杂芳基低级烷基或杂芳基低级烷酰基。 R2是氢，低级烷基，甲酰基或氰基; R3是氢或低级烷基; R4是低级烷基，芳基低级烷基，环烷基，芳基或杂芳基; 或者可选地，-NR 3 R 4一起构成R 5为氢，低级烷基，芳基，芳基低级烷基，杂芳基或杂芳基低级烷基，该化合物可用于治疗以胆碱能缺乏为特征的各种记忆功能障碍如阿尔茨海默氏病。

25. 发明授权

US4970218A N-(pyridinyl)-1H-indol-1-amines 失效
标题翻译： N-（吡啶基）-1H-吲哚-1-胺
公开(公告)号：US4970218A
公开(公告)日：1990-11-13
申请号：US405156
申请日：1989-09-11
申请人： Richard C. Effland , Joseph T. Klein , Larry Davis , Gordon E. Olsen
发明人： Richard C. Effland , Joseph T. Klein , Larry Davis , Gordon E. Olsen
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： There are disclosed compounds of the formula, ##STR1## where m, n, p, R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification; which compounds are useful for enhancing memory and also as analgesic and antidepressant agents.
摘要翻译：公开了下式的化合物，其中m，n，p，R，R 1，R 2和R 3如说明书中所定义; 哪些化合物可用于增强记忆力，也可用作镇痛药和抗抑郁药。

26. 发明授权

US4940704A Pyrido[3,4-b][1,4]benzoxazepines 失效
标题翻译：吡啶并[3,4-b] [1,4]苯并氧氮杂
公开(公告)号：US4940704A
公开(公告)日：1990-07-10
申请号：US394613
申请日：1989-08-16
申请人： Richard C. Effland , Joseph T. Klein
发明人： Richard C. Effland , Joseph T. Klein
IPC分类号： A61K31/55 , A61P25/04 , A61P25/24 , A61P25/26 , A61P25/28 , C07D498/04
CPC分类号： C07D498/04
摘要： Novel pyrido[3,4-b][1,4]benzoxazepines, intermediates for the preparation thereof, and methods for treating depression, alleviating pain, and relieving memory dysfunction are disclosed.
摘要翻译：公开了新颖的吡啶并[3,4-b] [1,4]苯并氧杂吖庚因，其制备中间体以及治疗抑郁症，减轻疼痛和缓解记忆功能障碍的方法。

27. 发明授权

US4935418A Medical compositions of 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines and use thereof 失效
标题翻译： 1-芳氧基-2,3,4,5-四氢-3-苯并氮杂的医药组合物及其用途
公开(公告)号：US4935418A
公开(公告)日：1990-06-19
申请号：US236104
申请日：1988-08-23
申请人： Richard C. Effland , Joseph T. Klein , Larry Davis
发明人： Richard C. Effland , Joseph T. Klein , Larry Davis
IPC分类号： C07D223/16
CPC分类号： C07D223/16
摘要： The invention relates to 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines of the formula ##STR1## wherein Y is the same or different and is hydrogen and lower alkoxy; X is hydrogen, halogen, lower alkyl, lower alkoxy, CF.sub.3, NO.sub.2, CN and NH.sub.2 ; R is hydrogen, lower alkyl, cycloalkyllower alkyl, ##STR2## Ar lower alkyl of the formula ##STR3## where Z is hydrogen, lower alkyl, lower alkoxy, halogen CF.sub.3, NO.sub.2 and NH.sub.2 ; Aryloxy lower alkyl of the formula ##STR4## where Z is as previously defined; and an alkylene amine of the formula ##STR5## where R.sub.1 and R.sub.2 are the same or different and are hydrogen and lower alkyl, n is an integer of 1 or 2; and the pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明涉及式（I）的1-芳氧基-2,3,4,5-四氢-3-苯并吖庚因，其中Y相同或不同，为氢和低级烷氧基; X是氢，卤素，低级烷基，低级烷氧基，CF 3，NO 2，CN和NH 2; R是氢，低级烷基，环烷基低级烷基，其中Z是氢，低级烷基，低级烷氧基，卤素，CF 3，NO 2和NH 2; 其中Z如前所定义的式“IMAGE”的芳氧基低级烷基; 和式“IMAGE”的亚烷基胺，其中R 1和R 2相同或不同，为氢和低级烷基，n为1或2的整数; 及其药学上可接受的酸加成盐。

28. 发明授权

US4916135A N-heteroaryl-4-quinolinamines 失效
标题翻译： N-杂芳基-4-喹啉胺
公开(公告)号：US4916135A
公开(公告)日：1990-04-10
申请号：US348937
申请日：1989-05-08
申请人： Richard C. Effland , Joseph T. Klein , Larry Davis , Gordon E. Olsen
发明人： Richard C. Effland , Joseph T. Klein , Larry Davis , Gordon E. Olsen
IPC分类号： A61K31/47 , A61P25/04 , A61P25/28 , C07D401/12
CPC分类号： C07D401/12
摘要： There are described compounds of the formula ##STR1## where --R is ##STR2## --R.sub.3 and R.sub.3 being independently --H, loweralkyl, --CHO, --CH.dbd.CH.sub.2, --CH.dbd.CH--loweralkyl, --CH.dbd.CHCO.sub.2 C.sub.2 H.sub.5, --CH.sub.2 N(C.sub.2 H.sub.5).sub.2 or ##STR3## --R.sub.1 when existent is --H, loweralkyl, --CH.sub.2 C.tbd.CH, ##STR4## R.sub.5 being methyl or phenyl optionally mono-substituted with loweralkyl or loweralkoxy;--R.sub.2 when existent is loweralkyl or --CH.sub.2 C.tbd.CH;--X is --H, loweralkyl, loweralkoxy, halogen or trifluoromethyl; and the two --Y groups when existent are both --H, or combine to constitute --(CH.sub.2).sub.4 --;which compounds are useful as analgesic agents, and for treating various memory dysfunctions characterized by decreased cholinergic function such as Alzheimer's disease.

29. 发明授权

US4806554A Pyrazol and indazolpyridinamines 失效
标题翻译：吡唑和吲唑吡啶胺
公开(公告)号：US4806554A
公开(公告)日：1989-02-21
申请号：US141852
申请日：1988-01-11
申请人： Richard C. Effland , Joseph T. Klein
发明人： Richard C. Effland , Joseph T. Klein
IPC分类号： C07D401/12 , A61K31/44 , A61K31/4427 , A61P25/04 , A61P25/24 , A61P25/26 , C07D401/04 , C07D521/00 , A61K31/415
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04
摘要： There are described compounds of the formula ##STR1## where n is 0 or 1; R.sub.1 is independently hydrogen, loweralkyl, loweralkenyl, loweralkynyl, loweralkoxycarbonylloweralkyl, loweralkylaminocarbonylloweralkyl, aminocarbonylloweralkyl, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl, loweralkylaminocarbonyl, arylloweralkylaminocarbonyl, arylaminocarbonyl, alkanoyl, arylloweralkanoyl, aroyl, alkenoyl, alkynoyl or --R.sub.5 --NR'R" where R.sub.5 is loweralkylene, loweralkenylene or loweralkynylene and R' and R" are each independently loweralkyl or alternatively the group --NR'R" as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-loweralkyl-1-piperazinyl or 4-aryl-1-piperazinyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 and R.sub.4 are each independently hydrogen or loweralkyl, or alternatively R.sub.3 and R.sub.4 taken together form --CH.dbd.CH--CH.dbd.CH-- so that the moiety ##STR2## becomes an indazole ring; and X is hydrogen, nitro, amino, halogen, loweralkanoylamino, arylloweralkanoylamino, aroylamino, alkylamino, arylloweralkylamino, loweralkyl, and cyano; which compounds are useful as analgesic and antidepressant agents.

30. 发明授权

US5296488A Method of using 2,3-dihydro-1-(pyridinylamino)-indoles as anticonvulsants and for the enhancement of memory 失效
标题翻译：使用2,3-二氢-1-（吡啶基氨基） - 吲哚作为抗惊厥药和增强记忆力的方法
公开(公告)号：US5296488A
公开(公告)日：1994-03-22
申请号：US972273
申请日：1992-11-05
申请人： Richard C. Effland , David G. Wettlaufer , Joseph T. Klein
发明人： Richard C. Effland , David G. Wettlaufer , Joseph T. Klein
IPC分类号： C07D401/12 , A61K31/44
CPC分类号： C07D401/12
摘要： This invention relates to 2,3-dihydro-1-(pyridinylamino)-indoles of the formula ##STR1## wherein R.sub.1 is hydrogen, loweralkyl, aryl, arylloweralkyl, alkenyl, alkynyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl; R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl, aryl, arylloweralkyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl; or R.sub.2 and R.sub.3 together form a cycloalkane ring of 4 to 6 carbons or a spiro-fused aryl or heteroaryl; the term heteroaryl signifying a group selected from pyridine or thiophene; X and Y are independently hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; m and n are independently integers of 1 to 3, or a pharmaceutically acceptable acid addition salt thereof or where appropriate, an optical, geometrical or stereoisomer or racemic mixture thereof. The compounds of this invention are useful as analgesics, anticonvulsants, and for the treatment of memory dysfunctions characterized by a cholinergic deficit.
摘要翻译：本发明涉及式IMA的2,3-二氢-1-（吡啶基氨基） - 吲哚，其中R 1是氢，低级烷基，芳基，芳基低级烷基，烯基，炔基或杂芳基低级烷基，其选自吡啶基甲基，吡啶基乙基，噻吩基甲基，噻吩乙基; R2和R3独立地是氢，低级烷基，芳基，芳基低级烷基或杂芳基低级烷基，选自吡啶基甲基，吡啶基乙基，噻吩基甲基，噻吩基乙基; 或R 2和R 3一起形成4至6个碳的环烷烃环或螺稠合的芳基或杂芳基; 表示选自吡啶或噻吩的基团的术语杂芳基; X和Y独立地是氢，卤素，羟基，低级烷基，低级烷氧基，硝基，氨基或三氟甲基; m和n独立地为1至3的整数，或其药学上可接受的酸加成盐，或适当时为其光学，几何或立体异构体或外消旋混合物。本发明的化合物可用作镇痛药，抗惊厥药，并用于治疗以胆碱能缺乏为特征的记忆功能障碍。

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